EP3476832B1 - Cationic lipid - Google Patents

Cationic lipid Download PDF

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Publication number
EP3476832B1
EP3476832B1 EP17815482.9A EP17815482A EP3476832B1 EP 3476832 B1 EP3476832 B1 EP 3476832B1 EP 17815482 A EP17815482 A EP 17815482A EP 3476832 B1 EP3476832 B1 EP 3476832B1
Authority
EP
European Patent Office
Prior art keywords
mmol
lipid
cationic lipid
compound
composition
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
EP17815482.9A
Other languages
German (de)
English (en)
French (fr)
Other versions
EP3476832A4 (en
EP3476832A1 (en
Inventor
Yuta Suzuki
Yoshinori Takahashi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eisai R&D Management Co Ltd
Original Assignee
Eisai R&D Management Co Ltd
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Publication of EP3476832A1 publication Critical patent/EP3476832A1/en
Publication of EP3476832A4 publication Critical patent/EP3476832A4/en
Application granted granted Critical
Publication of EP3476832B1 publication Critical patent/EP3476832B1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/7105—Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/713—Double-stranded nucleic acids or oligonucleotides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/28—Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Liposomes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
EP17815482.9A 2016-06-24 2017-06-22 Cationic lipid Active EP3476832B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2016125925 2016-06-24
PCT/JP2017/023051 WO2017222016A1 (ja) 2016-06-24 2017-06-22 カチオン性脂質

Publications (3)

Publication Number Publication Date
EP3476832A1 EP3476832A1 (en) 2019-05-01
EP3476832A4 EP3476832A4 (en) 2020-02-19
EP3476832B1 true EP3476832B1 (en) 2023-04-19

Family

ID=60784078

Family Applications (1)

Application Number Title Priority Date Filing Date
EP17815482.9A Active EP3476832B1 (en) 2016-06-24 2017-06-22 Cationic lipid

Country Status (15)

Country Link
US (1) US10501416B2 (ja)
EP (1) EP3476832B1 (ja)
JP (1) JP6883034B2 (ja)
KR (1) KR102358341B1 (ja)
CN (1) CN109311809B (ja)
AU (1) AU2017282459B2 (ja)
BR (1) BR112018075123A2 (ja)
CA (1) CA3020271A1 (ja)
ES (1) ES2948971T3 (ja)
IL (1) IL262574B (ja)
MX (1) MX2018015236A (ja)
RU (1) RU2740921C2 (ja)
SG (1) SG11201808928YA (ja)
TW (1) TWI745386B (ja)
WO (1) WO2017222016A1 (ja)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7164547B2 (ja) * 2017-12-27 2022-11-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 カチオン性脂質
CN110283223B (zh) * 2018-03-19 2022-01-04 广州市锐博生物科技有限公司 一种阳离子脂质分子及其在核酸递送中的应用
CN111164068B (zh) * 2018-08-21 2023-11-14 株式会社东芝 生物降解性化合物、脂质粒子、含有脂质粒子的组合物、及试剂盒
US10526603B1 (en) 2018-10-26 2020-01-07 Eisai R&D Management Co., Ltd. Double-stranded ribonucleic acid capable of suppressing expression of complement C5
JP6918197B2 (ja) * 2019-12-26 2021-08-11 エーザイ・アール・アンド・ディー・マネジメント株式会社 脂質複合体を含む医薬組成物及び脂質ナノ粒子を含む医薬組成物
KR20220122608A (ko) 2019-12-26 2022-09-02 에자이 알앤드디 매니지먼트 가부시키가이샤 보체 c5의 발현을 저해하는 이중 가닥 리보핵산을 함유하는 약제학적 조성물
WO2022168884A1 (ja) 2021-02-04 2022-08-11 塩野義製薬株式会社 カチオン性脂質
AU2022358609A1 (en) * 2021-09-28 2024-05-02 Seqirus Inc. Ionizable cationic compound
CN114213346B (zh) * 2022-02-22 2022-05-20 中国科学院基础医学与肿瘤研究所(筹) 一种双价可电离脂质化合物、组合物及其应用

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9139554B2 (en) 2008-10-09 2015-09-22 Tekmira Pharmaceuticals Corporation Amino lipids and methods for the delivery of nucleic acids
SI3431076T1 (sl) 2009-06-10 2022-04-29 Arbutus Biopharma Corporation Izboljšana lipidna formulacija
SG186085A1 (en) * 2010-06-03 2013-01-30 Alnylam Pharmaceuticals Inc Biodegradable lipids for the delivery of active agents
CN103167866B (zh) 2010-09-20 2015-09-23 瑟纳治疗公司 用于寡核苷酸递送的新型低分子量阳离子脂质
WO2012061259A2 (en) 2010-11-05 2012-05-10 Merck Sharp & Dohme Corp. Novel low molecular weight cyclic amine containing cationic lipids for oligonucleotide delivery
EP3960726A1 (en) 2011-10-18 2022-03-02 Dicerna Pharmaceuticals, Inc. Amine cationic lipids and uses thereof
CA2856742A1 (en) 2011-12-07 2013-06-13 Alnylam Pharmaceuticals, Inc. Biodegradable lipids for the delivery of active agents
WO2013135360A1 (en) * 2012-03-16 2013-09-19 Merck Patent Gmbh Aminoacid lipids
WO2013158579A1 (en) 2012-04-19 2013-10-24 Merck Sharp & Dohme Corp. Novel diester and triester based low molecular weight, biodegradable cationic lipids for oligonucleotide delivery
TW201726599A (zh) * 2012-07-06 2017-08-01 協和醱酵麒麟有限公司 陽離子性脂質
AU2013355258A1 (en) 2012-12-07 2015-06-11 Alnylam Pharmaceuticals, Inc. Improved nucleic acid lipid particle formulations
TW201534578A (zh) * 2013-07-08 2015-09-16 Daiichi Sankyo Co Ltd 新穎脂質
WO2015095351A1 (en) 2013-12-19 2015-06-25 Novartis Ag LEPTIN mRNA COMPOSITIONS AND FORMULATIONS
EP4019506A1 (en) 2013-12-19 2022-06-29 Novartis AG Lipids and lipid compositions for the delivery of active agents
TWI648067B (zh) * 2014-01-09 2019-01-21 日商衛材R&D企管股份有限公司 陽離子性脂質
KR20170023004A (ko) * 2014-06-30 2017-03-02 교와 핫꼬 기린 가부시키가이샤 양이온성 지질
TWI699354B (zh) 2014-12-26 2020-07-21 日商衛材R&D企管股份有限公司 陽離子性脂質

Also Published As

Publication number Publication date
JPWO2017222016A1 (ja) 2019-04-18
CN109311809B (zh) 2022-04-08
IL262574B (en) 2021-10-31
RU2018143237A3 (ja) 2020-07-24
EP3476832A4 (en) 2020-02-19
AU2017282459B2 (en) 2021-05-06
KR102358341B1 (ko) 2022-02-07
CN109311809A (zh) 2019-02-05
US20190218180A1 (en) 2019-07-18
AU2017282459A1 (en) 2018-11-01
ES2948971T3 (es) 2023-09-22
TW201803849A (zh) 2018-02-01
RU2740921C2 (ru) 2021-01-21
BR112018075123A2 (pt) 2019-06-18
EP3476832A1 (en) 2019-05-01
TWI745386B (zh) 2021-11-11
RU2018143237A (ru) 2020-07-24
MX2018015236A (es) 2019-04-11
US10501416B2 (en) 2019-12-10
IL262574A (en) 2018-12-31
JP6883034B2 (ja) 2021-06-02
WO2017222016A1 (ja) 2017-12-28
CA3020271A1 (en) 2017-12-28
KR20190021218A (ko) 2019-03-05
SG11201808928YA (en) 2018-11-29

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